Orlistat-d3 (Synonyms: (-)-Tetrahydrolipstatin-d3) |
| カタログ番号GC49236 |
オルリスタットの定量化のための内部標準
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1356930-46-5
Sample solution is provided at 25 µL, 10mM.
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Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor.1,2,3 It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM.4 It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner.5 Orlistat (10 mg/kg) decreases serum cholesterol levels and total body weight in a mouse model of obesity induced by a high-fat diet.6 Formulations containing orlistat have been used in the treatment of adult obesity.
1.Bisogno, T., Howell, F., Williams, G., et al.Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brainJ. Cell Biol.163(3)463-468(2003) 2.Hoover, H.S., Blankman, J.L., Niessen, S., et al.Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profilingBioorg. Med. Chem. Lett.18(22)5838-5841(2008) 3.Bustanji, Y., Issa, A., Mohammad, M., et al.Inhibition of hormone sensitive lipase and pancreatic lipase by Rosmarinus officinalis extract and selected phenolic constituentsJ. Med. Plant Res.4(21)2235-2242(2010) 4.Bisogno, T., Cascio, M.G., Saha, B., et al.Development of the first potent and specific inhibitors of endocannabinoid biosynthesisBiochim. Biophys. Acta1761(2)205-212(2006) 5.Kridel, S.J., Axelrod, F., Rozenkrantz, N., et al.Orlistat is a novel inhibitor of fatty acid synthase with antitumor activityCancer Res.64(6)2070-2075(2004) 6.Ji, W., Zhao, M., Wang, M., et al.Effects of canagliflozin on weight loss in high-fat diet-induced obese micePLoS One12(6)e0179960(2017)
| Cas No. | 1356930-46-5 | SDF | |
| 同義語 | (-)-Tetrahydrolipstatin-d3 | ||
| Canonical SMILES | [2H]C([2H])([2H])C(C)C[C@H](NC=O)C(O[C@@H](CCCCCCCCCCC)C[C@@H]1OC([C@H]1CCCCCC)=O)=O | ||
| Formula | C29H50D3NO5 | M.Wt | 498.8 |
| 溶解度 | Chloroform: slightly soluble,Methanol: slightly soluble | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0048 mL | 10.0241 mL | 20.0481 mL |
| 5 mM | 0.401 mL | 2.0048 mL | 4.0096 mL |
| 10 mM | 0.2005 mL | 1.0024 mL | 2.0048 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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